1 - 10 of 40 results
A fragment-based approach to protease inhibitor development. University of Antwerp
Active Center-Asisted Selection and Assembly (ACASA): a bottom-up approach to druglike protease inhibitors using caspase 4 as a model target. University of Antwerp
Development of photo-activatable protease inhibitors and activity-based probes and their application in the study of dynamic proteolytic processes KU Leuven
Proteases are involved in many highly regulated biological processes, such as apoptosis, cell-cell communication and blood coagulation. Inhibitors and activity-based probes (ABPs) have been successfully utilized as chemical tools to study these enzymes. However, when studying fast and dynamic processes, local and temporal acivation of these reagents is desirable. Such reagents can first of all be used for basic study of these processes, but ...
Validation of small molecule inhibitors of MALT1 protease for the treatment of auto-immune disorders and NF-κB-addicted lymphomas. KU Leuven
Current scientific literature highlights MALT1 protease activity as an important therapeutic target for treating NF-κB-mediated diseases such as autoimmune disorders and lymphoma. In collaboration with CD3 we have developed and patented three classes of MALT1 small molecule inhibitors that affect MALT1 substrate cleavage in cells and that reduce processes regulated by MALT1 protease activity such as IL2 production by and proliferation of ...
Active center assisted selection and assembly: a bottom-up approach to druglike protease inhibitors using urokinase plasminogen activator as a model target. University of Antwerp
Differential transcriptomics in the regulation of digestion and uptake of protease inhibitors in the desert locust, Schistocerca gregaria KU Leuven
Insects are among the most successful organisms on the planet. One explanation for their success is their extraordinary ability to successfully consume a wide range of foods. Like all heterotrophic organisms, insects need to acquire vital nutrients from their diet. The central organ for food digestion and absorption of nutrients is the gastrointestinal tract. This organ’s principal functions are to mediate the efficient digestion of food and ...
Optimization of the synthesis of diarylphosphonate inhibitors of serin proteases using reaction calorimetry. University of Antwerp
Study of the unfolded protein response in B-cell lymphoid malignancies and ynergism of proteasome inhibitores and pharmacological ER-stress inducers Ghent University
Proteasome inhibition is a new treatment modality for multiple myeloma and non-Hodgkin lymphoma. It is possible that manipulation of the unfolded protein response (UPR) can enhance and improve their treatment possibilities. Therefore the pro- and anti-apoptotic arms of the UPR will be mapped in lymphoma cell lines corresponding with the different stages of differentiation of the lymphocyte to plasma cell. Second the synergism of proteasome ...